Recent advances in our understanding of the structure and function of class B G protein-coupled receptors (GPCRs) provide multiple opportunities for targeted development of allosteric modulators. Given the pleiotropic signaling patterns emanating from these receptors in response to a variety of natural agonist ligands, modulators have the potential to sculpt the responses to meet distinct needs of different groups of patients. In this review, we provide insights into how this family of GPCRs differs from the rest of the superfamily, how orthosteric agonists bind and activate these receptors, the potential for allosteric modulators to interact with various regions of these targets, and the allosteric influence of endogenous proteins on the pharmacology of these receptors, all of which are important considerations when developing new therapies.

中文翻译：

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BG类蛋白偶联受体的变构调节的结构基础。

我们对BG类蛋白偶联受体（GPCR）的结构和功能的了解的最新进展为变构调节剂的靶向开发提供了多种机会。考虑到这些受体响应多种天然激动剂配体而产生的多效性信号传导模式，调节剂具有雕刻反应的潜力，以满足不同患者群体的不同需求。在本综述中，我们提供了有关此GPCR家族与其他超家族之间的区别，正构激动剂如何结合和激活这些受体，变构调节剂与这些靶标的各个区域相互作用的潜力以及内源性变构影响的见解。这些受体的药理学上的蛋白质，在开发新疗法时，所有这些都是重要的考虑因素。